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AR078012A1 - HETEROCICLIC DERIVATIVES OF PIRAZOL-4-IL-PIRROLO (2,3-D) PYRIMIDINS AS INHIBITORS OF THE QUANASA JANUS - Google Patents

HETEROCICLIC DERIVATIVES OF PIRAZOL-4-IL-PIRROLO (2,3-D) PYRIMIDINS AS INHIBITORS OF THE QUANASA JANUS

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Publication number
AR078012A1
AR078012A1 ARP100103190A ARP100103190A AR078012A1 AR 078012 A1 AR078012 A1 AR 078012A1 AR P100103190 A ARP100103190 A AR P100103190A AR P100103190 A ARP100103190 A AR P100103190A AR 078012 A1 AR078012 A1 AR 078012A1
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AR
Argentina
Prior art keywords
alkyl
heterocycloalkyl
heteroaryl
cycloalkyl
aryl
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Application number
ARP100103190A
Other languages
Spanish (es)
Inventor
Haisheng Wang
James D Rodgers
Yung-Long Li
Stacey Shepard
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Incyte Corp
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Publication of AR078012A1 publication Critical patent/AR078012A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente proporciona derivados heterocíclicos de las pirazol-4-il-pirrolo[2,3-d]pirimidinas, así como sus composiciones y métodos de uso, que modulan la actividad de las quinasas Janus (JAKs, por sus siglas en inglés) y son utiles en el tratamiento de enfermedades relacionadas con la actividad de las JAKs incluyendo, por ejemplo, trastornos inflamatorios, trastornos autoinmunes, cáncer, y otras enfermedades. Reivindicacion 1: Un compuesto que tiene la formula (1a) o una sal del mismo aceptable en el campo farmacéutico; en la cual: A es H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-14, heterocicloalquilo C2-13, arilo C6-14, heteroarilo C1-14, cicloalquilo C3-14-alquilo C1-4, heterocicloalquilo C2-13-alquilo C1-4, arilo C6-10-alquilo C1-4 o heteroarilo C1-14-alquilo C1-4, donde dicho alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-14, heterocicloalquilo C2-13, arilo C6-14, heteroarilo C1-14, cicloalquilo C3-14-alquilo C1-4, heterocicloalquilo C2-13-alquilo C1-4, arilo C6-10-alquilo C1-4 y heteroarilo C1-14-alquilo C1-4 están sustituido cada uno en forma opcional con 1, 2, 3, 4, 5 o 6 sustituyentes R8 seleccionados en forma independiente; Cada R8 está seleccionado en forma independiente a partir de halo, ciano, nitro, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-14, cicloalquilo C3-14-alquilo C1-4, heterocicloalquilo C2-14, heterocicloalquilo C2-14-alquilo C1-4, arilo C6-14, arilo C6-14-alquilo C1-4, heteroarilo C1-13, heteroarilo C1-13-alquilo C1-4, -ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)NReRf, -C(=O)Rb, -C(=O)ORb, -C(=O)NReRf, -OC(=O)Rb, -OC(=O)NReRf, -NReRf, -NRcC(=O)Rd, -NRcC(=O)ORd, -NRcC(=O)NRd, -NRcS(=O)2Rd, y -NRbS(=O)2NReRf; L está ausente C(=O), C(=O)NH, S(=O), o S(=O)2; X es CH o N; Y es H, ciano, halo, alquilo C1-4 o haloalquilo C1-4; Z es CR7 o N; R1, R2 y R3 son cada uno en forma independiente H, hidroxilo, halo, alquilo C1-3, o haloalquilo C1-3; R4 y R5 son cada uno independientemente H, alquilo C1-3 o haloalquilo C1-3; o R4 y R5 junto con el átomo de carbono al cual están unidos pueden formar un anillo cicloalquilo con 3-, 4-, 5- 6- o 7-miembros; cada R6 es en forma independiente hidroxilo, fluor, alquilo C1-4, hidroxi-C1-4-alquilo, alcoxi C1-4-alquilo C1-4, o fluor alquilo C1-4; R7 es H, fluor, alquilo C1-4 o fluor alquilo C1-4; Cada Ra, Rb, Rc, Rd, Re y Rf está seleccionado en forma independiente a partir de H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-4, heterocicloalquilo C2-7, heterocicloalquilo C2-7-alquilo C1-4, arilo C6-14, arilo C6-14-alquilo C1-4, heteroarilo C1-7, heteroarilo C1-7-alquilo C1-4; donde dicho alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-4, heterocicloalquilo C2-7, heterocicloalquilo C2-7-alquilo C1-4, arilo C6-14, arilo C6-14-alquilo C1-4, heteroarilo C1-7, y heteroarilo C1-7-alquilo C1-4 están cada uno opcionalmente sustituidos mediante 1, 2, 3 o 4 grupos seleccionados en forma independiente a partir de hidroxilo, halo, ciano, nitro, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 y di-C1-4-alquilamino; o cualquiera de Rc y Rd junto con la mitad a la cual están unidos, pueden formar un anillo heterociclo alquilo con 3-, 4-, 5-, 6- o 7-miembros opcionalmente sustituido con 1, 2, 3 o 4 grupos seleccionados en forma independiente a partir de hidroxilo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4y di-C1-4-alquilamino; o cualquiera de Re y Rf, junto con el átomo de nitrogeno al cual están unidos, pueden formar un anillo heterocicloalquilo o heteroarilo con 3-, 4-, 5-, 6- o 7-miembros, donde dicho anillo heterocicloalquilo o heteroarilo está sustituido opcionalmente con 1, 2, 3 o 4 grupos seleccionados en forma independiente a partir de hidroxilo, alquilo C1-4, haloalquilo C1-4, alcoxi C1-4, haloalcoxi C1-4, amino, alquilamino C1-4 y di-C1-4-alquilamino; m es 0 o 1; n es 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 o 10; y p es 0 o 1; a condicion de que no se exceda la valencia de cada átomo en las mitades opcionalmente sustituidas.This provides heterocyclic derivatives of pyrazol-4-yl-pyrrolo [2,3-d] pyrimidines, as well as their compositions and methods of use, which modulate the activity of Janus kinases (JAKs) and they are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. Claim 1: A compound having the formula (1a) or a salt thereof acceptable in the pharmaceutical field; in which: A is H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl, C1-14 heteroaryl, C3-14 cycloalkyl -4, C2-13 heterocycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl or C1-14 heteroaryl-C1-4 alkyl, wherein said C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl, C1-14 heteroaryl, C3-14 cycloalkyl-C1-4 alkyl, C2-13 heterocycloalkyl-C1-4 alkyl, C6-10 aryl-C1-4 alkyl and C1-14 heteroaryl-C1-4 alkyl are each optionally substituted with 1, 2, 3, 4, 5 or 6 independently selected R8 substituents; Each R8 is independently selected from halo, cyano, nitro, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-14 cycloalkyl, C3-14 cycloalkyl-C1-4 alkyl , C2-14 heterocycloalkyl, C2-14 heterocycloalkyl-C1-4 alkyl, C6-14 aryl, C6-14 aryl-C1-4 alkyl, C1-13 heteroaryl, C1-13 heteroaryl-C1-4 alkyl, -ORa, - SRa, -S (= O) Rb, -S (= O) 2Rb, -S (= O) NReRf, -C (= O) Rb, -C (= O) ORb, -C (= O) NReRf, -OC (= O) Rb, -OC (= O) NReRf, -NReRf, -NRcC (= O) Rd, -NRcC (= O) ORd, -NRcC (= O) NRd, -NRcS (= O) 2Rd , and -NRbS (= O) 2NReRf; L is absent C (= O), C (= O) NH, S (= O), or S (= O) 2; X is CH or N; Y is H, cyano, halo, C1-4 alkyl or C1-4 haloalkyl; Z is CR7 or N; R1, R2 and R3 are each independently H, hydroxyl, halo, C1-3 alkyl, or C1-3 haloalkyl; R4 and R5 are each independently H, C1-3 alkyl or C1-3 haloalkyl; or R4 and R5 together with the carbon atom to which they are attached can form a cycloalkyl ring with 3-, 4-, 5- 6- or 7-members; each R6 is independently hydroxyl, fluorine, C1-4 alkyl, hydroxy-C1-4-alkyl, C1-4 alkoxy-C1-4 alkyl, or fluorine C1-4 alkyl; R7 is H, fluorine, C1-4 alkyl or fluorine C1-4 alkyl; Each Ra, Rb, Rc, Rd, Re and Rf are independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3- cycloalkyl 7-C 1-4 alkyl, C 2-7 heterocycloalkyl, C 2-7 heterocycloalkyl-C 1-4 alkyl, C 6-14 aryl, C 6-14 aryl-C 1-4 alkyl, C 1-7 heteroaryl, C 1-7 heteroaryl-C 1-7 alkyl 4; wherein said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, C2-7 heterocycloalkyl, C2-7 heterocycloalkyl-C1- alkyl 4, C6-14 aryl, C6-14 aryl-C1-4 alkyl, C1-7 heteroaryl, and C1-7 heteroaryl-C1-4 alkyl are each optionally substituted by 1, 2, 3 or 4 groups independently selected from hydroxyl, halo, cyano, nitro, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, amino, C1-4 alkylamino and di-C1-4-alkylamino; or any of Rc and Rd together with the half to which they are attached, can form an alkyl heterocycle ring with 3-, 4-, 5-, 6- or 7-members optionally substituted with 1, 2, 3 or 4 groups selected independently from hydroxyl, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, amino, C1-4 alkylamino and di-C1-4-alkylamino; or any of Re and Rf, together with the nitrogen atom to which they are attached, can form a heterocycloalkyl or heteroaryl ring with 3-, 4-, 5-, 6- or 7-members, wherein said heterocycloalkyl or heteroaryl ring is substituted optionally with 1, 2, 3 or 4 groups independently selected from hydroxyl, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, C1-4 haloalkoxy, amino, C1-4 alkylamino and di-C1- 4-alkylamino; m is 0 or 1; n is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10; and p is 0 or 1; provided that the valence of each atom is not exceeded in the optionally substituted halves.

ARP100103190A 2009-09-01 2010-08-31 HETEROCICLIC DERIVATIVES OF PIRAZOL-4-IL-PIRROLO (2,3-D) PYRIMIDINS AS INHIBITORS OF THE QUANASA JANUS AR078012A1 (en)

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WO (1) WO2011028685A1 (en)

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